compound 6 / Pfizer - LARVOL DELTA

Synthesis and apoptotic induction of sulfonamide-based chalcone hybrids as first-in-class dual histone deacetylase‑carbonic anhydrase inhibitors with potential anti-tubulin activity. (PubMed, Bioorg Chem) - "Additionally, compounds 6a and 6e were found to be potent carbonic anhydrase inhibitors against the tested hCA isoforms, with inhibition constant (KIs) values mainly reaching a low nanomolar range (50.76-298.71 nM) compared to acetazolamide reference, beside their remarkable tubulin polymerization potential...Using a standard atomistic 100 ns dynamic simulation analysis, the stability of the complex formed between compound 6e and the HDAC2, CA-IX, and tubulin active sites was examined. Furthermore, the ADMET properties of 6e fulfilled Pfizer's criteria, demonstrating an optimal pharmacokinetic and safety profile."

Journal • Breast Cancer • Cervical Cancer • Colorectal Cancer • Lung Cancer • Oncology • Solid Tumor • BCL2 • CA9 • CASP7 • CASP9 • HDAC2